| 摘要 |
Piperidine compounds having the general general Formula I <CHEM> wherein R<1> is a) a group consisting of alkyl, alkenyl, cycloalkyl, cycloalkenyl, phenyl, cycloalkylalkyl, cycloalkenylalkyl, phenylalkyl or diphenylalkyl linked to the piperidyl N-atom through an at least 2 membered spacer group or; b) a group having the general Formula II : <CHEM> wherein X is CHR<1><0>, O, S, SO, SO2 or NR<1><0>, R<1><0> being hydrogen, alkyl or alkenyl, an amino group, sulfonyl, optionally substituted phenyl or a hetero aromatic group; Y is CH, CH2, NH, C=O or C=S; R<a> - R<d> are substituents; U is CH2, O or S; Q<1> is a bond , alkylene or alkenylen and Q<2> alkylene having at least two C-atoms or alkenylene R<2> and R<3> are hydrogen, or alkyl or they may together form an ethylene or propylene bridge; R<4> to R<7> are substituents; and i) Z<1> and Z<2> are linked together in which case: Z<1> is CH2, O or S; Z<2> and Z<3> are independently (CH2)n, n being 0 or 1, O or S or Z<1> and Z<2> may together represent a group -CH=CH-; or when Z<3> is (CH2)n wherein n is 0, Z<1> and Z<2> may together represent a 3-membered divalent group; or ii) when R<1> is a group as defined in b) Z<1> and Z<2> may also be unlinked, in which case: Z<1> is substituent, Z<2> is hydrogen and Z<3> is (CH2)n wherein n is 0; show potent sigma receptor activity. Furthermore they show effect in animal models indicative of anxiolytic properties. Accordingly they are useful as medicines for the treatment of anxiety, psychosis, epilepsy, convulsion, movement disorders, motor disturbances, amnesia, cerebrovascular diseases, senile dementia of the Alzheimer type or Parkinson's disease. |
